4-(Piperidin-1-yl)aniline → (2S,4S)-4-fluoro-1-[[N-[4-[N-(4-piperidinylphenyl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]pyrrolidine-2-carbonitrile

HRID 228028

반응식

HRID 228028 반응식
[C:1]([C:4]12[CH2:11][CH2:10][C:7]([NH:12][CH2:13][C:14]([N:16]3[CH2:20][C@@H:19]([F:21])[CH2:18][C@H:17]3[C:22]#[N:23])=[O:15])([CH2:8][CH2:9]1)[CH2:6][CH2:5]2)([OH:3])=O.[NH2:24][C:25]1[CH:30]=[CH:29][C:28]([N:31]2[CH2:36][CH2:35][CH2:34][CH2:33][CH2:32]2)=[CH:27][CH:26]=1>>[F:21][C@@H:19]1[CH2:20][N:16]([C:14](=[O:15])[CH2:13][NH:12][C:7]23[CH2:10][CH2:11][C:4]([C:1]([NH:24][C:25]4[CH:26]=[CH:27][C:28]([N:31]5[CH2:36][CH2:35][CH2:34][CH2:33][CH2:32]5)=[CH:29][CH:30]=4)=[O:3])([CH2:5][CH2:6]2)[CH2:9][CH2:8]3)[C@H:17]([C:22]#[N:23])[CH2:18]1

참가 물질

3

반응물 2

HCID 4135014-(Piperidin-1-yl)anilineHCID 57634365(2S,4S)-1-[[N-(4-carboxybicyclo[2,2,2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile

생성물 1

HCID 57756857(2S,4S)-4-fluoro-1-[[N-[4-[N-(4-piperidinylphenyl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]pyrrolidine-2-carbonitrile수율 19.6%

실험 절차

In a similar manner to Example 63, (2S,4S)-1-[[N-(4-carboxybicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (50.0 mg) and N-(4-aminophenyl)piperidine (61.4 mg) were used to obtain (2S,4S)-4-fluoro-1-[[N-[4-[N-(4-piperidinylphenyl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]pyrrolidine-2-carbonitrile (14.6 mg).

출처 및 근거

ORD 기록
ord-0e990551bf114d7fa04613718aa3609e
출처 데이터셋
uspto-grants-2009_07
특허 번호
US07560569B2

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